. Author manuscript; available in PMC: 2017 Apr 26.

Published in final edited form as: Biochemistry. 2016 Apr 15;55(16):2390–2400. doi: 10.1021/acs.biochem.6b00012

Table 1.

Comparison of the inhibition of mature PR^S17 and PR, and autoprocessing of TFR-PR^S17 precursor at the p6pol/PR^S17 site, with a panel of clinical inhibitors. The inhibitors are listed in the order of increasing K_i (decreasing affinity) for PR^S17. Estimated K_i values for wild-type PR from published sources are listed here solely for comparison. Similar values from different sources were averaged. In the present work K_i values for inhibition of mature PR^S17 were determined by ITC or by kinetic analysis as indicated by superscripts ITC and K, respectively.

Protease inhibitor (PI)	Inhibition of PR^S17K_i (nM)	Inhibition of PR K_i (nM)	Relative resistance (PR^S17/PR)	Inhibition of autoprocessing at p6pol-PR^S17site IC₅₀ (μM)	Difference in inhibition [autoprocessing, IC₅₀/mature PR^S17, K_i]
APV	11 ± 3.1^ITC	0.20^a	55	7.5	682
DRV	50 ± 8.3^ITC	0.005^b	10000	15	300
ATV	70 ± 14^K	0.035^c	2000	15	214
LPV	73 ± 20^K	0.02^a,c	3650	~60	822
IDV	810 ± 75^ITC	0.25^c	3240	~50	62
NFV	5870 ± 1730^K	0.36^a,b,d	16300	>42	>7.2
RTV	6360 ± 1310^K	0.064^a,d	99380	~105	16.5
SQV	8390 ± 2640^K	0.39^a,b,d	21500	>105	>12.5

^a,b,c,d

K_i values are cited from references^48–50,30, respectively, for comparison with PR^S17. K_i values cited in reference⁵⁰ were determined by kinetics and the rest by ITC.